Synthesis of conformationally constrained benzoylureas as BH3-mimetics
Details
Publication Year 2012, Volume 10, Issue #27, Page 5230-5237
Journal Title
ORGANIC & BIOMOLECULAR CHEMISTRY
Publication Type
Journal Article
Abstract
The design of small molecules that mimic the BH3 domain and bind to Bcl-2 proteins has emerged as a promising approach to discovering novel anti-cancer therapeutics. We reveal the design and synthesis of conformationally constrained benzoylurea scaffolds as conformational probes. Central to helix mimicry, the intramolecular hydrogen bond in the benzoylurea plays a key role in the pre-organisation of the acyclic substrates for cyclisation via ring closing metathesis, providing efficient access to the constrained mimetics.
Publisher
ROYAL SOC CHEMISTRY
Keywords
OXYGEN CHANNELING ASSAY; CELL-SURVIVAL; APOPTOSIS; BCL-2; COMPLEX; FAMILY; REGULATORS; SWITCH
Rights Notice
© Royal Society of Chemistry 2013


Creation Date: 2012-01-01 12:00:00
Last Modified: 0001-01-01 12:00:00
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